Open AccessInhibition of Compound 48/80-Mediated Histamine Release from Isolated Rat Mast Cells by Oosponol-Related Compounds (4-Acyl-Isocoumarins).
Author(s) -
Masayasu Kimura,
Isami Waki,
Mitsunori Kokubo
Publication year - 1978
Publication title -
japanese journal of pharmacology/japanese journal of pharmacology
Language(s) - English
Resource type - Journals
eISSN - 1347-3506
pISSN - 0021-5198
DOI - 10.1254/jjp.28.693
Subject(s) - histamine , compound 48/80 , isocoumarins , chemistry , isocoumarin , pharmacology , mast cell , stereochemistry , biochemistry , biology , immunology , degranulation , receptor , catalysis
Oosponol (4-hydroxymethylketone-8-hydroxyisocoumarin) is a metabolic product isolated from Oospora astringens which originated from house dust in a room of an asthmatic patient. The compound and the structurally related isocoumarins were studied to determine the inhibition of histamine release induced by compound 48/80 from isolated rat peritoneal mast cells. The released histamine was assayed by fluorometry. The compounds tested were not observed to release histamine. Some of 4-acyl-isocoumarins inhibited the histamine release at doses less than 10 micrometers, whereas the 3-acyl- and the 4-alkyl-compounds were not effective at doses over 100 microns. The pretreatment of mast cell with the compound for 15 min before the application of compound 48/80 was more effective than the simultaneous administration. The mode of inhibitory action of KIT-302, 4-(4'-carboxy-benzoyl)-isocoumarin, was non-competitive antagonism to compound 48/80 on the mast cells.